title: Antiobesity designed multiple ligands: Synthesis of pyrazole fatty acid amides and evaluation as hypophagic agents.
abstract: Searching for new antiobesity agents, a new series of fatty acid amide derivatives of 1,5-diarylpyrazole have been synthesized as dual peroxisome proliferator activated receptor alpha (PPARalpha)/cannabinoid receptor ligands. The compounds have been evaluated in vivo and in vitro as PPARalpha activators and as cannabinoids in two tests of the mouse tetrad. In vivo, food intake studies have been performed with all the compounds. No significant cannabinoid activity has been found but some compounds behaved as potent PPARalpha activators. Several compounds showed anorexigenic properties reducing food intake in rats.
authors.affiliation: Instituto de Química Médica, CSIC, Juan de la Cierva 3, 28006 Madrid, Spain.
authors.forename: Mario
authors.initials: M
authors.lastname: Alvarado
authors.forename: Pilar
authors.initials: P
authors.lastname: Goya
authors.forename: Manuel
authors.initials: M
authors.lastname: Macías-González
authors.forename: Francisco Javier
authors.initials: FJ
authors.lastname: Pavón
authors.forename: Antonia
authors.initials: A
authors.lastname: Serrano
authors.forename: Nadine
authors.initials: N
authors.lastname: Jagerovic
authors.forename: Jose
authors.initials: J
authors.lastname: Elguero
authors.forename: Angel
authors.initials: A
authors.lastname: Gutiérrez-Rodríguez
authors.forename: Santiago
authors.initials: S
authors.lastname: García-Granda
authors.forename: Margarita
authors.initials: M
authors.lastname: Suardíaz
authors.forename: Fernando
authors.initials: F
authors.lastname: Rodríguez de Fonseca
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D019440:Anti-Obesity Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002186:Cannabinoids / Q000737:chemistry / Q000378:metabolism; D004435:Eating; D005227:Fatty Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D005982:Glutathione Transferase / Q000378:metabolism; D051379:Mice; D047493:PPAR alpha / Q000819:agonists* / Q000378:metabolism; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar
chemical_list: D000577:Amides; D019440:Anti-Obesity Agents; D002186:Cannabinoids; D005227:Fatty Acids; D047493:PPAR alpha; D011720:Pyrazoles; D005982:Glutathione Transferase